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SIM1

Catalog #: 7432 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7432/5
SIM1 | CAS No. 2719051-84-8 | Active Degraders
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Description: Potent and selective trivalent BET Bromodomain Degrader (PROTAC®)

Chemical Name: N,N'-(11-((2-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide)

Purity: ≥98%

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Biological Activity

SIM1 is a potent and selective trivalent PROTAC® Degrader based on BET bromodomain inhibitors linked to a Von Hippel Lindau (VHL) ligand via branched linkers. SIM1 degrades all BET family proteins with a preference for BRD2 (DC50 values = 0.7 nM, 1.1 nM and 3.3 nM for BRD4, BRD2 and BRD3, respectively). SIM1 degrades BRD2 more significantly and rapidly than BRD3 and BRD4, and degrades BET proteins with a higher potency than a bivalent degrader. SIM1 also decreases protein levels for Myc and HMOX1 and induces apoptosis in prostate cancer cells.

Technical Data

M.Wt:
1618.82
Formula:
C79H98Cl2N14O13S3
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2719051-84-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under licence from the University of Dundee

Product Datasheets

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